Penthorum chinense Pursh (Ganhuangcao), a traditional Chinese medicine, is used for the prevention and treatment of liver diseases, including hepatitis B, hepatitis C, and alcoholic liver damage. A wide range of investigations have been carried out on this herbal medicine from pharmacognosy to pharmaceuticals, as well as pharmacology. The extract of P. chinense was reported to have significant liver protective effects through anti-oxidation, reduction of key enzyme levels, inhibition of hepatitis B virus DNA replication, and promotion of bile secretion. Based on the current knowledge, flavonoids and phenols are considered to be responsible for P. chinense's bioactivities. The main purpose of this review is to provide comprehensive and up-to-date knowledge of the phytochemical and pharmacological studies performed on P. chinenseduring the past few decades. Moreover, it intends to provide new insights into the research and development of this herbal medicine.